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Items: 48

1.

Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor.

Janes MR, Zhang J, Li LS, Hansen R, Peters U, Guo X, Chen Y, Babbar A, Firdaus SJ, Darjania L, Feng J, Chen JH, Li S, Li S, Long YO, Thach C, Liu Y, Zarieh A, Ely T, Kucharski JM, Kessler LV, Wu T, Yu K, Wang Y, Yao Y, Deng X, Zarrinkar PP, Brehmer D, Dhanak D, Lorenzi MV, Hu-Lowe D, Patricelli MP, Ren P, Liu Y.

Cell. 2018 Jan 25;172(3):578-589.e17. doi: 10.1016/j.cell.2018.01.006.

PMID:
29373830
2.

Oncogenic Characterization and Pharmacologic Sensitivity of Activating Fibroblast Growth Factor Receptor (FGFR) Genetic Alterations to the Selective FGFR Inhibitor Erdafitinib.

Karkera JD, Cardona GM, Bell K, Gaffney D, Portale JC, Santiago-Walker A, Moy CH, King P, Sharp M, Bahleda R, Luo FR, Alvarez JD, Lorenzi MV, Platero SJ.

Mol Cancer Ther. 2017 Aug;16(8):1717-1726. doi: 10.1158/1535-7163.MCT-16-0518. Epub 2017 Apr 17.

3.

Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor.

Perera TPS, Jovcheva E, Mevellec L, Vialard J, De Lange D, Verhulst T, Paulussen C, Van De Ven K, King P, Freyne E, Rees DC, Squires M, Saxty G, Page M, Murray CW, Gilissen R, Ward G, Thompson NT, Newell DR, Cheng N, Xie L, Yang J, Platero SJ, Karkera JD, Moy C, Angibaud P, Laquerre S, Lorenzi MV.

Mol Cancer Ther. 2017 Jun;16(6):1010-1020. doi: 10.1158/1535-7163.MCT-16-0589. Epub 2017 Mar 24.

4.

A Novel Bispecific Antibody Targeting EGFR and cMet Is Effective against EGFR Inhibitor-Resistant Lung Tumors.

Moores SL, Chiu ML, Bushey BS, Chevalier K, Luistro L, Dorn K, Brezski RJ, Haytko P, Kelly T, Wu SJ, Martin PL, Neijssen J, Parren PW, Schuurman J, Attar RM, Laquerre S, Lorenzi MV, Anderson GM.

Cancer Res. 2016 Jul 1;76(13):3942-53. doi: 10.1158/0008-5472.CAN-15-2833. Epub 2016 May 23.

5.

Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.

Wan H, Schroeder GM, Hart AC, Inghrim J, Grebinski J, Tokarski JS, Lorenzi MV, You D, Mcdevitt T, Penhallow B, Vuppugalla R, Zhang Y, Gu X, Iyer R, Lombardo LJ, Trainor GL, Ruepp S, Lippy J, Blat Y, Sack JS, Khan JA, Stefanski K, Sleczka B, Mathur A, Sun JH, Wong MK, Wu DR, Li P, Gupta A, Arunachalam PN, Pragalathan B, Narayanan S, K C N, Kuppusamy P, Purandare AV.

ACS Med Chem Lett. 2015 Jul 12;6(8):850-5. doi: 10.1021/acsmedchemlett.5b00226. eCollection 2015 Aug 13.

6.

Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.

Hart AC, Schroeder GM, Wan H, Grebinski J, Inghrim J, Kempson J, Guo J, Pitts WJ, Tokarski JS, Sack JS, Khan JA, Lippy J, Lorenzi MV, You D, McDevitt T, Vuppugalla R, Zhang Y, Lombardo LJ, Trainor GL, Purandare AV.

ACS Med Chem Lett. 2015 Jul 10;6(8):845-9. doi: 10.1021/acsmedchemlett.5b00225. eCollection 2015 Aug 13.

7.

9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.

Zimmermann K, Sang X, Mastalerz HA, Johnson WL, Zhang G, Liu Q, Batt D, Lombardo LJ, Vyas D, Trainor GL, Tokarski JS, Lorenzi MV, You D, Gottardis MM, Lippy J, Khan J, Sack JS, Purandare AV.

Bioorg Med Chem Lett. 2015 Jul 15;25(14):2809-12. doi: 10.1016/j.bmcl.2015.04.101. Epub 2015 May 11.

PMID:
25987372
8.

Selective JAK2/ABL dual inhibition therapy effectively eliminates TKI-insensitive CML stem/progenitor cells.

Lin H, Chen M, Rothe K, Lorenzi MV, Woolfson A, Jiang X.

Oncotarget. 2014 Sep 30;5(18):8637-50.

9.

Dysregulated STAT1-SOCS1 control of JAK2 promotes mammary luminal progenitor cell survival and drives ERĪ±(+) tumorigenesis.

Chan SR, Rickert CG, Vermi W, Sheehan KC, Arthur C, Allen JA, White JM, Archambault J, Lonardi S, McDevitt TM, Bhattacharya D, Lorenzi MV, Allred DC, Schreiber RD.

Cell Death Differ. 2014 Feb;21(2):234-46. doi: 10.1038/cdd.2013.116. Epub 2013 Sep 13.

10.

Tumor grafts derived from patients with head and neck squamous carcinoma authentically maintain the molecular and histologic characteristics of human cancers.

Peng S, Creighton CJ, Zhang Y, Sen B, Mazumdar T, Myers JN, Lai SY, Woolfson A, Lorenzi MV, Bell D, Williams MD, Johnson FM.

J Transl Med. 2013 Aug 27;11:198. doi: 10.1186/1479-5876-11-198. Erratum in: J Transl Med. 2014;12:67. Lai, Stephen Y [added].

11.

Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2.

Purandare AV, McDevitt TM, Wan H, You D, Penhallow B, Han X, Vuppugalla R, Zhang Y, Ruepp SU, Trainor GL, Lombardo L, Pedicord D, Gottardis MM, Ross-Macdonald P, de Silva H, Hosbach J, Emanuel SL, Blat Y, Fitzpatrick E, Taylor TL, McIntyre KW, Michaud E, Mulligan C, Lee FY, Woolfson A, Lasho TL, Pardanani A, Tefferi A, Lorenzi MV.

Leukemia. 2012 Feb;26(2):280-8. doi: 10.1038/leu.2011.292. Epub 2011 Oct 21.

PMID:
22015772
12.

Drug discovery approaches to target Wnt signaling in cancer stem cells.

Curtin JC, Lorenzi MV.

Oncotarget. 2010 Nov;1(7):563-577. Review.

13.

Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.

Harikrishnan LS, Kamau MG, Wan H, Inghrim JA, Zimmermann K, Sang X, Mastalerz HA, Johnson WL, Zhang G, Lombardo LJ, Poss MA, Trainor GL, Tokarski JS, Lorenzi MV, You D, Gottardis MM, Baldwin KF, Lippy J, Nirschl DS, Qiu R, Miller AV, Khan J, Sack JS, Purandare AV.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1425-8. doi: 10.1016/j.bmcl.2011.01.022. Epub 2011 Jan 11.

PMID:
21282055
14.

Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)--Hit to Lead studies.

Wan H, Huynh T, Pang S, Geng J, Vaccaro W, Poss MA, Trainor GL, Lorenzi MV, Gottardis M, Jayaraman L, Purandare AV.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5063-6. doi: 10.1016/j.bmcl.2009.07.040. Epub 2009 Jul 10.

PMID:
19632837
15.

Kinase drug discovery approaches in chronic myeloproliferative disorders.

Kumar C, Purandare AV, Lee FY, Lorenzi MV.

Oncogene. 2009 Jun 18;28(24):2305-13. doi: 10.1038/onc.2009.107. Epub 2009 May 4. Review.

PMID:
19421140
16.

Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1).

Huynh T, Chen Z, Pang S, Geng J, Bandiera T, Bindi S, Vianello P, Roletto F, Thieffine S, Galvani A, Vaccaro W, Poss MA, Trainor GL, Lorenzi MV, Gottardis M, Jayaraman L, Purandare AV.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):2924-7. doi: 10.1016/j.bmcl.2009.04.075. Epub 2009 Apr 22.

PMID:
19419866
17.

Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA.

Kim SH, Tokarski JS, Leavitt KJ, Fink BE, Salvati ME, Moquin R, Obermeier MT, Trainor GL, Vite GG, Stadnick LK, Lippy JS, You D, Lorenzi MV, Chen P.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):634-9. Epub 2007 Nov 28.

PMID:
18055203
18.

Constitutively active receptor tyrosine kinases as oncogenes in preclinical models for cancer therapeutics.

Kellar KA, Lorenzi MV, Ho CP, You D, Wen ML, Ryseck RP, Oppenheimer S, Fink BE, Vite GD, Rowley BR, Yu C, Bol DK, Lee FY, Wong TW.

Mol Cancer Ther. 2006 Jun;5(6):1571-6.

19.

Identification of a novel series of tetrahydrodibenzazocines as inhibitors of 17beta-hydroxysteroid dehydrogenase type 3.

Fink BE, Gavai AV, Tokarski JS, Goyal B, Misra R, Xiao HY, Kimball SD, Han WC, Norris D, Spires TE, You D, Gottardis MM, Lorenzi MV, Vite GD.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1532-6. Epub 2006 Jan 4.

PMID:
16386902
20.

Identification of novel functional inhibitors of 17beta-hydroxysteroid dehydrogenase type III (17beta-HSD3).

Spires TE, Fink BE, Kick EK, You D, Rizzo CA, Takenaka I, Lawrence RM, Ruan Z, Salvati ME, Vite GD, Weinmann R, Attar RM, Gottardis MM, Lorenzi MV.

Prostate. 2005 Oct 1;65(2):159-70.

PMID:
15924334
21.

Synthetic lethality of retinoblastoma mutant cells in the Drosophila eye by mutation of a novel peptidyl prolyl isomerase gene.

Edgar KA, Belvin M, Parks AL, Whittaker K, Mahoney MB, Nicoll M, Park CC, Winter CG, Chen F, Lickteig K, Ahmad F, Esengil H, Lorenzi MV, Norton A, Rupnow BA, Shayesteh L, Tabios M, Young LM, Carroll PM, Kopczynski C, Plowman GD, Friedman LS, Francis-Lang HL.

Genetics. 2005 May;170(1):161-71. Epub 2005 Mar 2.

22.

Deregulation and mislocalization of the cytokinesis regulator ECT2 activate the Rho signaling pathways leading to malignant transformation.

Saito S, Liu XF, Kamijo K, Raziuddin R, Tatsumoto T, Okamoto I, Chen X, Lee CC, Lorenzi MV, Ohara N, Miki T.

J Biol Chem. 2004 Feb 20;279(8):7169-79. Epub 2003 Nov 25.

23.

Rho exchange factor ECT2 is induced by growth factors and regulates cytokinesis through the N-terminal cell cycle regulator-related domains.

Saito S, Tatsumoto T, Lorenzi MV, Chedid M, Kapoor V, Sakata H, Rubin J, Miki T.

J Cell Biochem. 2003 Nov 1;90(4):819-36.

PMID:
14587037
24.

Selective retinoids and rexinoids in cancer therapy and chemoprevention.

Zusi FC, Lorenzi MV, Vivat-Hannah V.

Drug Discov Today. 2002 Dec 1;7(23):1165-74. Review. Erratum in: Drug Discov Today. 2003 Oct 1;8(19):877.

PMID:
12547017
25.

Tumor necrosis factor-alpha induces the expression of DR6, a member of the TNF receptor family, through activation of NF-kappaB.

Kasof GM, Lu JJ, Liu D, Speer B, Mongan KN, Gomes BC, Lorenzi MV.

Oncogene. 2001 Nov 29;20(55):7965-75.

26.

Synergistic cytotoxicity exhibited by combination treatment of selective retinoid ligands with taxol (Paclitaxel).

Vivat-Hannah V, You D, Rizzo C, Daris JP, Lapointe P, Zusi FC, Marinier A, Lorenzi MV, Gottardis MM.

Cancer Res. 2001 Dec 15;61(24):8703-11.

27.

Ostip2, a novel oncoprotein that associates with the Rho exchange factor Ost.

Yamanaka R, Blumenthal R, Lorenzi MV, Tatsumoto T, Miki T.

DNA Cell Biol. 2001 Jul;20(7):383-90.

PMID:
11506702
28.

The RIP-like kinase, RIP3, induces apoptosis and NF-kappaB nuclear translocation and localizes to mitochondria.

Kasof GM, Prosser JC, Liu D, Lorenzi MV, Gomes BC.

FEBS Lett. 2000 May 19;473(3):285-91.

29.

Neu differentiation factor/heregulin induction by hepatocyte and keratinocyte growth factors.

Castagnino P, Lorenzi MV, Yeh J, Breckenridge D, Sakata H, Munz B, Werner S, Bottaro DP.

Oncogene. 2000 Feb 3;19(5):640-8.

30.

Homocysteine exerts cell type-specific inhibition of AP-1 transcription factor.

Suzuki YJ, Lorenzi MV, Shi SS, Day RM, Blumberg JB.

Free Radic Biol Med. 2000 Jan 1;28(1):39-45.

PMID:
10656289
31.

Human FRAG1 encodes a novel membrane-spanning protein that localizes to chromosome 11p15.5, a region of frequent loss of heterozygosity in cancer.

Lorenzi MV, Castagnino P, Aaronson DC, Lieb DC, Lee CC, Keck CL, Popescu NC, Miki T.

Genomics. 1999 Nov 15;62(1):59-66.

PMID:
10585768
32.
34.

Distinct expression patterns and transforming properties of multiple isoforms of Ost, an exchange factor for RhoA and Cdc42.

Lorenzi MV, Castagnino P, Chen Q, Hori Y, Miki T.

Oncogene. 1999 Aug 19;18(33):4742-55.

35.

Human T-cell lymphotropic/leukemia virus type 1 Tax abrogates p53-induced cell cycle arrest and apoptosis through its CREB/ATF functional domain.

Mulloy JC, Kislyakova T, Cereseto A, Casareto L, LoMonico A, Fullen J, Lorenzi MV, Cara A, Nicot C, Giam C, Franchini G.

J Virol. 1998 Nov;72(11):8852-60.

36.

Assignment of the ect2 protooncogene to mouse chromosome band 3B by in situ hybridization.

Takai S, Lorenzi MV, Long JE, Yamada K, Miki T.

Cytogenet Cell Genet. 1998;81(1):83-4. No abstract available.

PMID:
9691182
37.
38.

Ligand-independent activation of fibroblast growth factor receptor-2 by carboxyl terminal alterations.

Lorenzi MV, Castagnino P, Chen Q, Chedid M, Miki T.

Oncogene. 1997 Aug 14;15(7):817-26.

39.

Cooperative transformation of NIH3T3 cells by G alpha12 and Rac1.

Tolkacheva T, Feuer B, Lorenzi MV, Saez R, Chan AM.

Oncogene. 1997 Aug 7;15(6):727-35.

40.

FRAG1, a gene that potently activates fibroblast growth factor receptor by C-terminal fusion through chromosomal rearrangement.

Lorenzi MV, Horii Y, Yamanaka R, Sakaguchi K, Miki T.

Proc Natl Acad Sci U S A. 1996 Aug 20;93(17):8956-61.

41.

Expression of an ATP binding mutant of PKC-delta inhibits Sis-induced transformation of NIH3T3 cells.

Li W, Michieli P, Alimandi M, Lorenzi MV, Wu Y, Wang LH, Heidaran MA, Pierce JH.

Oncogene. 1996 Aug 15;13(4):731-7.

PMID:
8761294
42.

A 15 amino acid stretch close to the Grb2-binding domain defines two differentially expressed hSos1 isoforms with markedly different Grb2 binding affinity and biological activity.

Rojas JM, Coque JJ, Guerrero C, Aroca P, Font de Mora J, de la Cruz X, Lorenzi MV, Esteban LM, Santos E.

Oncogene. 1996 Jun 6;12(11):2291-300.

PMID:
8649768
43.

Inhibition of oncogene-mediated transformation by ectopic expression of p21Waf1 in NIH3T3 cells.

Michieli P, Li W, Lorenzi MV, Miki T, Zakut R, Givol D, Pierce JH.

Oncogene. 1996 Feb 15;12(4):775-84.

PMID:
8632899
44.

The human choline acetyltransferase gene encodes two proteins.

Grosman DD, Lorenzi MV, Trinidad AC, Strauss WL.

J Neurochem. 1995 Aug;65(2):484-91.

PMID:
7616201
45.

Expression cloning, developmental expression and chromosomal localization of fibroblast growth factor-8.

Lorenzi MV, Long JE, Miki T, Aaronson SA.

Oncogene. 1995 May 18;10(10):2051-5.

PMID:
7761105
46.

Two mRNAs are transcribed from the human gene for choline acetyltransferase.

Lorenzi MV, Trinidad AC, Zhang R, Strauss WL.

DNA Cell Biol. 1992 Oct;11(8):593-603.

PMID:
1388731
47.

Nerve growth factor regulation of choline acetyltransferase gene expression in rat embryo basal forebrain cultures.

Lorenzi MV, Knusel B, Hefti F, Strauss WL.

Neurosci Lett. 1992 Jun 22;140(2):185-8.

PMID:
1380145
48.

Tetrahydroaminoacridine and other allosteric antagonists of hippocampal M1 muscarine receptors.

Potter LT, Ferrendelli CA, Hanchett HE, Hollifield MA, Lorenzi MV.

Mol Pharmacol. 1989 May;35(5):652-60.

PMID:
2725474

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